BRPI0616532A2 - method for suppressing, repelling or inhibiting biting mosquitoes and gnats and composition for releasing an effective amount of a repressor, repellent, inhibitor compound - Google Patents

Abstract

METHOD FOR REPRESSING, REPELLING OR INHIBITING MOSQUITOES AND MOSQUITOES-PóLVORA BITERS AND COMPOSITION TO RELEASE AN EFFECTIVE AMOUNT OF A REPRESSOR, REPELLENT, INHIBITOR COMPOUND. Certain components of citrus fruits and limonene oxidation products are effective repressors, repellents and / or space inhibitors for mosquitoes and powder-biting mosquitoes. The repressive, repellent and / or inhibitor compounds for mosquitoes and mosquito-biting mosquitoes are nerile acetate, citronellar acetate, geranyl acetate, hydroxy-p-cymene, citral, cc-terpineol, citronelal, linaloyl acetate , citronelol, terpen-4-ol, tetrahydrocarvone, oxidized limonene products including d-carvone, 1-carvone, (+) limonene oxide, (-) limonene oxide, cis and trans carveol, a diol and an aldehyde, and mixtures thereof.

Description

"METHOD FOR REPRESSING, REPELLING OR INHIBITING MOSQUITOS IN POWDER MOTORS AND COMPOSITION FOR RELEASING AN EFFECTIVE AMOUNT OF A REPELLANT, REPELLENT, INHIBITOR COMPOUND".

Field of the invention

The invention relates to improved compounds, compositions and systems for preventing or repelling biting mosquitoes and gnats from a target, or providing a facial inhibitor to prevent mosquitoes and biting gnats from perceiving or landing on a target, particularly a human target. The invention also provides a method for employing such compounds and compositions to prevent or repel target contact mosquitoes and mosquitoes or to inhibit them from perceiving or landing on a target.

Invention History

In the field of mosquito repellent and control of biting gnats, many compounds or substances have been employed. For example, DEET® has been used as a mosquito repellent and biting mosquito repellent. However, DEET® is a contact repellent that mosquitoes or gnats avoid when they come in contact with such a repellent. Thus, DEET® is applied to a person's skin to repel mosquitoes or gunpowder when they contact DEET®.

However, for many people DEET® can have irritating or toxic effects and cannot be applied to their skin. Citronella oil also showed relatively low efficacy for its intended use as a space inhibitor. Recently, it has been found that certain 3-methyl-1-alken-3-ols, such as linalol, act as space inhibitors, that is, these compounds inhibit the ability of multipurpose mosquitoes to perceive a human target when these compounds are dispersed in an environment. .

It has been observed that, in general, certain bird mammals will slip or clean their skin or skin with fruits, leaves, or other parts of plants with a clear purpose to suppress ectoparasites, a phenomenon known as anointing. For this purpose many animalists have used lemons (Citrus limina), limes (Citrusaurantilolia) and other citrus fruits as deformation materials. In many cases, peels, oils or fragrances of these fruits are applied by animals to their skin or skin for this purpose of suppressing parasites. The major or major component of these citrus fruits is limonene (4-isopropenyl-1-methylcyclohexane) generally more than 55% and usually about 95% -99% in the peel of these fruits. From this it is assumed or inferred that limonene may be an effective spatial repellent or inhibitor to mosquitoes. However when tested or limonene against mosquitoes it was found to be neither effective nor as repellent as a spatial inhibitor.

In view of the potential toxic and irritating effects of DEET® there is a need for other naturally occurring and naturally occurring space repressors, repellents and / or mosquito gunpowder inhibitors that provide low risk to consumers and users of such products.

Summary of the invention

Certain components of citrus fruits, skins, peels or epicarps and d-limonene oxidation products contained in the fruit, as well as some closely related materials, have been found to be effective as parasquite and mosquito-powder spatial inhibitors, repellents and / or inhibitors. Accordingly, according to this invention there is provided a method for suppressing, repelling or inhibiting mosquitoes and spotted mosquitoes of a human or environmental area, the method comprising providing the human or environmental area with an effective amount to suppress / repel / inhibit at least one animal. compound selected from neryl acetate, citronellyl acetate, geranyl acetate, 8-hydroxy-p-cymene, citral, α-terpineol, citronellal, delinaloyl acetate, citronellol, terpen-4-ol, tetrahydrocarvone, oxidized limonene products, and mixtures thereof, with the proviso that for use as a mosquito bite repressor / repellent in a human being, citral is not employed as the only compound / repellent or spatial repressor / inhibitor of the compound group. Oxidized limonene products include, but are not limited to d- and 1-carvone, (+) limonene oxide, (-) limonene oxide, useful and trans carveol, a diol and an aldehyde.

The compounds which have been found to be contact repellers / mosquito repellents in biting mosquitoes, feeding mosquitoes and biting mosquito repellants, particularly effective are neril acetate, citronellyl acetate, geranyl acetate, hydroxy-p-cymene, citral, α -terpineol, citronellal, linaloyl acetate, citronelol, d- and 1-carvone, (+) limonene oxide, (-) limonene oxide, eis and trans carveol, terpen-4-ol, tetrahydrocarvone and mixtures thereof with As a condition for use as a mosquito bite repressor / repellent in a human being, the citral is not employed as the sole repressor / repellent component.

The compounds neryl acetate, citronellyl acetate, geranyl acetate, citral, α-terpineol, citronellal, citronellol, (+) / (-) limonene oxide, oxidized limonene products, particularly d-carvone, 1- carvone, and lo and trans carveol, and mixtures thereof are particularly effective as spatial repellents / inhibitors for mosquitoes and gnats. The compounds neryl acetate, hydroxy-p-cymene, citronellal, linaloyl acetate, geranyl acetate, α-terpineol, d-carvone, 1-carvone, (+) and (-) delimonene oxide, useful and trans carveol, tetrahydrocarvone They are especially effective contact repellents / repressors of mosquitoes and gnats. The compounds may be formulated in suitable carriers as topical repressive, repellent or inhibitor compositions. The use of the compounds of this invention for the above inhibitory and repelling purposes is, for example, but not limited to the following methods. To repel mosquitoes and toadstools from a human being, the method comprises applying to the skin of a human a repellent effective amount of at least one compound, selected from neryl deacetate, hydroxy-p-cymene, citral, citronellal acetate linaloyl, geranyl acetate, α-terpineol, tetrahydrocarvone, oxidized limonene products and mixtures thereof with the condition that for use as a mosquito repressor and mosquito-powder repellent in a human being, citral is not employed as the only repressor / repellent compound thereof decomposed group, and citronellal is not employed as the sole repressor / repellent or facial repressor / inhibitor compound of this group of compounds. For use as a space repellent / inhibitor the method comprises distributing in an environmental area where such inhibitory effect is desired to be provided, an effective inhibitory amount of at least one compound selected from neryl acetate, citronellyl acetate, geranyl acetate, 8-hydroxy-p-cymene, citral, α-terpineol, citronellal, citronellol, linaloyl acetate, terpen-4-ol, limonene oxide products, and mixtures thereof. Dispensing may be by evaporation of a vehicle compound, dispersion by an aerosol, or incorporation of the compounds into granules or powders which may be dispersed in the powder, and the like.

Brief Description of Drawings

Figure 1 is a graph of the feeding results (feed suppression or contact repellency) of mosquitoes for compounds (citrus oil components) of this invention against control when tested in the examples. Figure 2 is a graph of the flight results (repelling or spatial inhibition). ) for control compounds (citrus oil components) of this invention when tested in the examples.

Figure 3 is a graph of the feed results (feed suppression or contact repellency) of mosquitoes for compounds (delimonene oxidation products) of this invention against control when tested in the examples.

Figure 4 is a graph of the flight (spatial repellency) results for compounds (delimonene oxidation products) of this invention against control when tested in the examples.

Figure 5 is a graph of spatial inhibition / inhibition results (% of mosquitoes caught) of mosquitoes caught in an "American Biophysics Mosquito Magnet Liberty Plus" mosquito trap relative to a control without the repellent compounds of this invention.

Detailed Description of the Invention and Preferred Embodiments

According to this invention it has been found that certain citrus fruit components and delimonene oxidation products are effective as spatial repressors, repellents and / or inhibitors of mosquitoes and mosquitoes. The compounds which are feed suppressants or contact repellents for biting mosquitoes and / or biting mosquito repellants and / or space biting mosquito repellants are found to be neryl acetate, decitronellil acetate, geranyl acetate, hydroxy-p-cymene , citral, α-terpineol, citronellal, citronellol, delinaloyl acetate, terpen-4-ol, tetrahydrocarvone, oxidised delimonene products, and mixtures thereof, provided that they are used as a repressor / repellent for biting mosquitoes, not used citral as the only repressor / repellent or spatial repressor / inhibitor compound of this group of compounds. Oxidized limonene products include, but are not limited to, d-carvone and 1-carvone, (+) limonene oxide, (-) limonene oxide, useful and trans carveol, a diol and an aldehyde. The compounds neryl acetate, citronellyl acetate, geranyl acetate, hydroxy-p-cymene, citral, α-terpineol, terpen-4-ol, citronellal, citronelol, d-carvone, 1-carvone, eis and trans carveol, linaloyl acetate, (+) / (-) limonene oxide, mixtures thereof are particularly effective as spatial inhibitors for mosquitoes and it has been found that the compounds of neryl acetate, hydroxy-p-cymene, citral, citronellal acetate linaloyl, geranyl acetate, citronelol, α-terpineol, d-carvone, 1-carvone, eis carransol, (+) and (-) limonene oxide, and mixtures thereof are especially effective as contact demosquito repellents. The compounds may be formulated in appropriate repellent, repressor compositions or in space inhibitory compositions.

For mosquito repellent and mosquito-repellent mosquitoes, the repellent compounds of this invention may be formulated in any compositions suitable for application of an effective repellent amount of the repellent compound to a human skin, typically in an amount ranging from 0.5% to 75% by weight. of composition. For spatial inhibition of the ability of biting mosquitoes and mosquitoes to perceive a target, the inhibitor compounds of this invention may be formulated into any suitable composition to spread an effective spatial inhibitory amount of the inhibitor compound in an environmental area in which spatially inhibiting mosquitoes and mosquitoes are desired to perceive their targets. . This effective inhibitory amount will typically range from 0.000005-0.010gram / hour / ft2 of the base area of the environmental area in which inhibition is sought.

It is understood that the active compounds of this invention may be employed in combination with other components recognized as repressors, repellents and / or inhibitors, such as including, but not limited to, those repellent spatial inhibitor compounds disclosed for example in US Patent No. 6,362,235, and in US Patent Application No. US 2005 / 0090563Al. A preferred inhibitor compound which may be combined with the repressor, repellent and / or inhibitor compounds of this invention is linalol, and especially d-linalol (which is also found in citrus fruits).

The repressor / repellant / inhibitor compounds of this invention may be synthesized or obtained from natural oils, such as, for example, including but not limited to: coriander, mint, citronella, caraway, and similar.

The repressor / repellant / inhibitor compounds of this invention may be formulated as hereinbefore described in any appropriate release system or means. For example, the formulated composition may be formulated in a suitable vehicle or release system, including but not limited to release systems such as heated or unheated evaporative devices such as candles or compositions placed on a fan-driven apparatus, floor or carpet laying compositions or floor compositions. , ankle or wrist band compositions or the like, and absorbent material compositions which may be spread on the floor or floor. The many other ways in which the active compounds of this invention may be released will be readily apparent to those skilled in the art. Thus, the invention comprises a para-deliberative composition of a repressive / repellent / inhibitor effective amount of a mosquito or biting mosquito repellent / inhibitor effective compound, said composition comprising (a) at least one compound selected from the group consisting of neryl acetate, acetate decitronellil, geranyl acetate, 8-hydroxy-p-cymene, citral, α-terpineol, citronellal, citronellol, delinaloyl acetate, terpen-4-ol, tetrahydrocarvone, oxidized delimonene products including d- and 1-carvone, (+) oxide delimonene, (-) limonene oxide, eis and trans carveol, umiol and an aldehyde, and mixtures thereof, with the proviso that for use as a mosquito bite or mosquito repellent / repellent in a human being, do not appear to be citral as the sole repressor / repellant compound of this group of compounds, and citronellal is not employed as the sole repressor, repellant or inhibitor of this group of compounds; and (b) a carrier vehicle for releasing said at least one compound to a human or an environment.

The following tests were employed to illustrate the effectiveness of the compounds of this invention in effectively acting as mosquito repressors, repellents or space inhibitors. The test was performed at 900-2100 hours in a sufficiently large incubator (26 ° C, 63-80% relative humidity (HR)) illuminated by fluorescent lamps. Mosquitoes were tested on a two-piece Pexiglas module designed to assess their response to feeding repressors. The bottom of the module was a 40 χ 7 χ 4 cm platformhock supporting six circular cavities (diameter = 3.8 cm; depth = 6 mm). Water (at 40 ° C) flowed through the central well of the platform at a rate of 215 mL / min. The top piece of the module consisted of six 4.5 χ 4.0 χ 5.0 cm chambers, the floors of which were fitted with a sliding door positioned over a 3.5 cm diameter circular opening. Mosquitoes were introduced through a 1 cm diameter opening in the front wall of the chambers. For each test, five female mosquitoes (Aedes aegypti) were aspirated into each of the five chambers of the top module piece and the openings were closed with stoppers wrapped in plastic pellets. The wells in the low-modulus specimen were filled with 7 mL of 10% sucrose solution containing ATP (2.9 mg / mL). In each well 75 μl of green dye (McCormick Food, Hunt Valley, MD) were added so that those mosquitoes that drunk the sugar solution could be identified when crushed at the end of the tests. Each membrane received 50 μΐι of acetone or experimental compound solution, applied over a 9.6 cm2 circular area to 1 mm thick membranes made of nylon mesh in a silicone matrix. The membranes were then placed over each well in contact with the sugar solution.

The circular openings in the floor of each chamber of the module part were aligned with each membrane-covered cavity of the lower part. The sliding floors of the chambers were then opened allowing mosquitoes to access the membranes. The number of mosquitoes that landed on the membranes, and those that flew inside the apparatus, were recorded every minute for five minutes. After five minutes, any mosquitoes that remained on the membranes were removed with a phytometallic, and the floor door of each chamber was closed. The module's top side was then placed in a freezer for minutes. In the test designed to evaluate feeding, mosquitoes were removed from the frozen module, crushed on white paper towels, and examined for the presence of green dye to indicate that feeding had occurred. Bottle-fed mosquito ratios were analyzed using a standard generalized modelolinear with a logit binding.

Measurements of landing and flight counts are repeated; Five readings were obtained for groups of five mosquitoes. Consequently, to maintain independence among the data, the five readings were summed, and then the sums divided by 25 (the maximum count in each category) to create proportions of landing and flying mosquitoes. The proportions were then transferred using the standard variance stabilizing transform to proportions (sin "1 / y, where y is the ratio), and analyzed using ANOVA (variable analysis).

The results of the feed tests are shown in Figures 1 and 3. In the graphs of Figures 1 and 3, the lower the proportion of feed compared to the control (1.00) is indicative of the increased repellent activity of the tested compounds. The flight test results are shown in Figures 2 and 4. In the graphs of Figures 2 and 4, the higher the flight number in relation to control (1) is indicative of the increased inhibitory activity of the tested compounds. The compounds neryl acetate, citronellyl acetate, geranyl acetate, hydroxy-p-cymene, citral, α-terpineol, terpen-4-ol, citronellal, citronellol, d-carvone, 1-carvone, linaloyl acetate were found. , (+) / (-) limonene oxide, and oxidized limonene products, and mixtures thereof are particularly effective as spatial inhibitors for mosquitoes and it has been found that deneryl, citral, citronellal acetate, linaloyl acetate, geranyl acetate, hydroxy-β- cymene, α-terpineol, d-carvone, 1-carvone, (+) and (-) oxidized limonene oxide and tetrahydrocarvone elimonene and mixtures thereof are especially effective as contact mosquito repellents. The ability of compounds of this invention has been demonstrated. spatially inhibit the ability of mosquitoes to perceive an outdoor target through the following example.

Pieces of absorbing material absorbed two grams of decomposed test. These pieces of absorbent material (Rhopore Inc. fragrance release material) containing the absorbed test material were deposited in a stream of CO2 and r-octenol and released from an "American Biophysics Mosquito Magnet Liberty Plus" mosquito trap designed to attract mosquitoes. The test was performed over a period of 2-5 days in such a way that both the control (same test compound trap) and the test compound were tested in equal numbers of times on each employed trap. The number of mosquitoes caught in the test compound traps was compared to the number of mosquitoes caught in the trap with no test compound present. That is, mosquitoes caught with the control were considered as 100% catch and the handle with the detest material was calculated as a percentage of mosquitoes caught relative to the control. Thus, a decreased percentage is indicative of the increased ability of test compounds to inhibit mosquitoes' ability to perceive the target. The results are shown in the Table of Figure 5. For 1-carvone, 1-carvone mixed with known spatial inhibitors d-linalol, citral, citronellal, d-carvone the percentage of mosquitoes caught relative to the control was in the range of about 6-8%. , indicating an inhibition of more than 90% of the ability of the mosquitoes to perceive the target trap. Somewhat effective but still effective inhibitors were 8-hydroxy-β-cymene (about 34% relative handle), terpen-4-ol (about 38% relative handle), useful and trans carveol (about 43%). relative grip) and tetrahydrocarvone (about 52% relative grip).

For mosquito repellent, the compounds of this invention may be applied to the skin of a human in any amount of effective repellent. For spatial inhibition of mosquitoes' ability to sense a target, and for spatial appearance, the compounds of this invention may be delivered to the atmosphere in any effective amount.

While the invention has been described herein with reference to specific embodiments thereof, it will be understood that exchanges, modifications and variations may be made without departing from the spirit and scope of the inventive concept disclosed herein. Accordingly, it is intended to encompass all such exchanges, modifications and variations that fall within the spirit and scope of the appended claims.

Claims (14)

1. Method for suppressing, repelling or inhibiting mosquitoes in biting mosquitoes of a human or environmental area, which comprises applying to the human or environmental area an effective repressive, repellent, inhibitory amount of at least one compound selected from the group consisting of deneryl acetate, citronellyl acetate, geranyl acetate, 8-hydroxy-p-cymene, citral, linaloyl acetate, terpen-4-ol, tetrahydrocarvone, oxidized limonene products including d-carvone, 1-carvone, (+) oxide (-) limonene oxide, eis and trans carveol, a diol and an aldehyde, and mixtures thereof, with the proviso that I use as a repressor, biting mosquito repellent in a human being, do not appear to be citrated like single repressive compound, repellent from this group of compounds. Method according to claim 1, characterized in that it comprises applying to the human skin a repressive effective amount, repellent of at least one repressor compound, selected group repellent consisting of neryl acetate, citronellyl acetate, geranyl acetate, hydroxy -p-cymene, citral, delinaloyl acetate, d-carvone and 1-carvone, (+) limonene oxide, (-) limonene oxide, eis and trans carveol, terpen-4-ol, tetrahydrocarvone, and mixtures thereof, with the condition that citral should not be used as the only repellent, repellent of this group. A method according to claim 2, characterized in that the at least one repellent, repellent compound is selected from the group consisting of 1-carvone, d-carvone, and transcarveol and mixtures thereof. Method according to any one of claims 1, 2 or 3, characterized in that an additional repressor-repellent compound is applied in combination as at least one repellent-repellent compound. Method according to claim 4, characterized in that the additional repellent-repressor compound is d-linalol. Method according to any one of claims 1 to 5, characterized in that it is for suppressing, repelling mosquitoes. A method according to claim 1 for inhibiting the ability of mosquitoes to perceive a human target in an environmental area, comprising spreading in an environmental area where such inhibitory effect is desired to provide an inhibitory effective amount of at least one group-selected inhibitor compound. neryl acetate, citronellyl acetate, geranyl acetate, hydroxy-p-cymene, citral, delinaloyl acetate, terpen-4-ol, tetrahydrocarvone, oxidized delimonene products including d-carvone, 1-carvone, (+) limonene oxide, (-) Useful limonene oxide and transcarveol, a diol and an aldehyde, and mixtures thereof. A method according to claim 7, characterized in that the at least one inhibitor compound is selected from the group consisting of d-carvone, 1-carvone, useful and trans carveol, and mixtures thereof. Method according to any one of claims 7 and 8, characterized in that an additional inhibitor compound is spread in combination with the at least one inhibitor compound. Method according to any one of claims 7, 8 and 9, characterized in that the additional inhibitory compound is d-linalol. Method according to any one of claims 7 to 10, characterized in that it is for inhibiting mosquitoes. 12. Composition for the release of an effective amount of a repressor, repellent, inhibitor effective counter-mosquito or biting mosquito, characterized in that it comprises (a) at least one selected compound from the group consisting of neryl acetate, citronellyl acetate, geranyl acetate. , 8-hydroxy-p-cymene, citral, linaloyl acetate, terpen-4-ol, tetrahydrocarvone, oxidized limonene products inclusiveived-carvone, 1-carvone, (+) limonene oxide, (-) delimonide oxide, eis and trans carveol, a diol and an aldehyde, in mixtures thereof, with the proviso that for use as a repressor, mosquito repellent, and mosquito-repellent mosquito in a human being, citral is not employed as the only repressor, repellent, or spatial inhibitor compound of this group of compounds; and (b) a carrier vehicle for releasing said at least one compound into a human or environment. Composition according to Claim 12, characterized in that the at least one compound comprises a compound selected from the group consisting of d-carvone, 1-carvone, useful and trans carveol, and mixtures thereof. Composition according to any one of Claims 12 and 13, characterized in that it further comprises d-linalol.